2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU6028418

VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4.

For research use only. We do not sell to patients.

VU6028418 Chemical Structure

VU6028418 Chemical Structure

CAS No. : 2649803-05-2

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Based on 1 publication(s) in Google Scholar

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Description

VU6028418 is a potent, highly selective and orally bioavailable M4 mAChR antagonist with an IC50 of 4.1 nM against hM4[1].

IC50 & Target

mAChR4

 

In Vivo

VU6028418 is orally bioavailable[1].
In Vivo PK Parameters for VU6028418[1]

parameter rat
(SD)a		 mouse
(CD-1)a		 dog
(beagle)a
dose (mg/kg) iv/po 1/10 1/3 1/3
CLp (mL/min/kg) 6.1 17 43
Vss (L/kg) 6.7 10.6 8.5
elimination t1/2 (h) 13 NC 15
Cmax (ng/mL) po 17 000 181 70
Tmax (h) po 1.5 6.67 17
AUC0-inf (ng/mL•h) po 30 000 NC 1100
F (%) po ≥100 ≥100 86
total brain/total plasma (Kp) 6.4 ND ND
unbound brain/unbound plasma
(Kp,uu)		 0.61 ND ND
CSF/plasma unbound (Kp,u) 0.24 ND ND

a Values represent means from two to three animals. ND = not determined. NC = not calculated; there was insufficient data to define the elimination phase (i.e., Cmax was one of the last three time points).

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD rat, CD-1 mouse and beagle dog[1]
Dosage: 1, 3 and 10 mg/kg
Administration: Intravenous injection or oral administration (Pharmacokinetic Analysis)
Result: Showed good pharmacokinetic results.
Molecular Weight

432.48

Formula

C23H27F3N4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC(F)=C(F)C(C2=CC=C(N[C@H]3C[C@@](CN(CC4CCOCC4)C5)([H])[C@@]5([H])C3)N=N2)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 5.56 mg/mL (12.86 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3122 mL 11.5612 mL 23.1225 mL
5 mM 0.4624 mL 2.3122 mL 4.6245 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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(per animal)

g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3122 mL 11.5612 mL 23.1225 mL 57.8061 mL
5 mM 0.4624 mL 2.3122 mL 4.6245 mL 11.5612 mL
10 mM 0.2312 mL 1.1561 mL 2.3122 mL 5.7806 mL
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VU6028418 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU60284182649803-05-2VU 6028418VU-6028418mAChRMuscarinic acetylcholine receptororally bioavailableInhibitorinhibitorinhibit

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